Amino-substituted tetracyclic compounds

Abstract

The invention discloses novel compounds of the general formula: ##STR1## and salts thereof, in which X stands for oxygen, sulphur, the group >NR 7 or the group --CR 8 R 9 --; R 1 , r 2 , r 3 and R 4 represent hydrogen, hydroxy, halogen, alkyl (1-6 C), alkoxy (1-6 C), alkylthio (1-6 C) or trifluoromethyl; R 5 and R 6 represent hydrogen, alkyl (1-6 C), aralkyl (7-10 C) or together in combination with the nitrogen atom a heterocyclic five- or six-membered ring; R 7 stands for hydrogen or alkyl (1-4 C); R 8 and R 9 stand for hydrogen or methyl, n is the number 0, 1 or 2 and The dotted line means an optional C--C bond, With valuable central nervous system (CNS) activities, especially antidepressant activity.

I claim: 
     
       1. A compound of the formula: ##STR18## or a pharmaceutically acceptable salt thereof, in which X represents the group consisting of oxygen and sulphur, R 1 , r 2 , r 3  and R 4  are selected from the group consisting of hydrogen, hydroxy, halogen, alkyl having 1 to 6 carbon atoms, alkoxy having 1 to 6 carbon atoms, alkylthio having 1 to 6 carbon atoms and trifluoromethyl,   R 5 , r 6  are selected from the group consisting of hydrogen, alkyl having 1 to 6 carbon atoms, aralkyl having 7 to 10 carbon atoms, and together in combination with the nitrogen atom a morpholine ring,   n is selected from 0, 1 and 2, and   the dotted line signifies an optional bond.   
     
     
       2. A compound according to claim 1 of the formula I A: ##STR19## in which R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , X and n have the meanings indicated in claim 1. 
     
     
       3. A compound of the formula I according to claim 1 in which n is the number 0 or 1. 
     
     
       4. The compound of claim 1 wherein R 6  is selected from the group consisting of hydrogen and alkyl having 1 to 6 carbon atoms. 
     
     
       5. The compound of claim 1 which is 2-dimethylamino-1,2,3,4-tetrahydro-tribenzo-(b,d,f)-oxepine. 
     
     
       6. The compound of claim 1 which is 2-amino-1,2,3,4-tetrahydro-tribenzo(b,d,f)-oxepine. 
     
     
       7. The compound of claim 1 which is 2-amino-11-trifluoromethyl-1,2,3,4-tetrahydro-tribenzo(b,d,f)-oxepine. 
     
     
       8. The compound of claim 1 which is 2-amino-11-methyl-1,2,3,4-tetrahydro-tribenzo(b,d,f)-oxepine. 
     
     
       9. The compound of claim 1 which is 2-amino-12-chloro-1,2,3,4-tetrahydro-tribenzo(b,d,f)-oxepine. 
     
     
       10. The compound of claim 1 which is 2-dimethylamino-6-chloro-1,2,3,4-tetrahydro-tribenzo(b,d,f)-oxepine. 
     
     
       11. The compound of claim 1 which is 2-dimethylamino-12-chloro-1,2,3,4-tetrahydro-tribenzo(b,d,f)-oxepine. 
     
     
       12. The compound of claim 1 which is 2-dimethylamino-11-methyl-1,2,3,4-tetrahydro-tribenzo(b,d,f)-oxepine. 
     
     
       13. The compound of claim 1 which is 2-dimethylamino-11,12-dimethyl-1,2,3,4-tetrahydro-tribenzo(b,d,f)-oxepine. 
     
     
       14. The compound of claim 1 which is 2-dimethylamino-6-methyl-1,2,3,4-tetrahydro-tribenzo(b,d,f)-oxepine. 
     
     
       15. The compound of claim 1 which is 2-dimethylamino-11-trifluoromethyl-1,2,3,4-tetrahydro-tribenzo(b,d,f)-oxepine. 
     
     
       16. The compound of claim 1 which is 2-methylamino-1,2,3,4-tetrahydro-tribenzo(b,d,f)-oxepine. 
     
     
       17. The compound of claim 1 which is 2-dimethylamino-1,2,3,4-tetrahydro-tribenzo(b,d,f)-oxepine. 
     
     
       18. The compound of claim 1 which is 2-aminoethyl-1,2,3,4-tetrahydro-tribenzo(b,d,f)-oxepine. 
     
     
       19. The compound of claim 1 which is 2-aminomethyl-1,2,3,4-tetrahydro-tribenzo(b,d,f)-oxepine. 
     
     
       20. The compound of claim 1 which is 2-dimethylaminomethyl-1,2,3,4-tetrahydro-tribenzo(b,d,f)-oxepine. 
     
     
       21. The compound of claim 1 which is 2-amino-1,2,3,4,4a,13b-hexahydro-tribenzo(b,d,f)-oxepine. 
     
     
       22. The compound of claim 1 which is 2-dimethylamino-1,2,3,4a,13b-hexahydro-tribenzo(b,d,f)-oxepine. 
     
     
       23. The compound of claim 1 which is 2-methylamino-1,2,3,4,4a,13b-hexahydro-tribenzo(b,d,f)-oxepine. 
     
     
       24. The compound of claim 1 which is 2-amino-1,2,3,4-tetrahydro-tribenzo(b,d,f)-thiepine. 
     
     
       25. The compound of claim 1 which is 2-dimethylamino-1,2,3,4-tetrahydro-tribenzo(b,d,f)-thiepine. 
     
     
       26. The compound of claim 1 which is 2-morpholino-1,2,3,4-tetrahydro-tribenzo(b,d,f)-oxepine. 
     
     
       27. The compound of claim 1 which is 2-morpholino-1,2,3,4-tetrahydro-tribenzo(b,d,f)-thiepine.